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drug screening tests

Syed Beenish Rufai, Jitendra Singh, Parveen Kumar, Purva Mathur, Sarman Singh
There is limited data on the use of Genotype MTBDRslVersion 1 (MTBDRsl V1) as an initial rapid screening test to rule out XDR-TB and most importantly its performance in various genotypes of Mycobacterium tuberculosis is scarcely studied. A total of 359 MDR-TB isolates were tested for gene mutations representing second line drug resistance, using the MTBDRsl_V.1 and the results were compared with phenotypic method (Bactec MGIT-960 system) for second-line drug (SLD) susceptibility testing. Genetic lineages of all these isolates were also determined using spoligotyping and SITVIT2 WEB database...
June 18, 2018: Scientific Reports
Mohamed El-Naggar, Hadia Almahli, Hany S Ibrahim, Wagdy M Eldehna, Hatem A Abdel-Aziz
In our endeavor towards the development of effective anticancer agents, a novel series of pyridine-ureas 8a ⁻ n were synthesized. All the newly prepared derivatives were evaluated in vitro for their growth inhibitory activity towards the proliferation of breast cancer MCF-7 cell line. Compounds 8e and 8n were found to be the most active congeners against MCF-7 cells (IC50 = 0.22 and 1.88 µM after 48 h treatment; 0.11 and 0.80 µM after 72 h treatment, respectively) with increased activity compared to the reference drug doxorubicin (IC50 = 1...
June 15, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Outi Vainio
Background and purpose The use of laboratory animals in pain research has powerfully contributed to our detailed understanding of the physiological mechanisms of pain. Animal models also represent an essential tool to screen and select novel drug molecules with potentially analgesic properties. Despite of the inevitable input of laboratory animal trials, recent studies have shown that animal pain models have repeatedly failed to predict clinical analgesic efficacy and adverse side effects of potential drug molecules in human pain patients...
December 29, 2017: Scandinavian Journal of Pain
Yuan Zhang, Vijai Kumar Reddy Tangadanchu, Rammohan R Yadav Bheemanaboina, Yu Cheng, Cheng-He Zhou
A series of carbazole-triazole conjugates were designed, synthesized and characterized by IR, NMR, and HRMS spectra. Biological assay showed that most of the synthesized compounds exhibited moderate and even strong antifungal activities, especially 3,6-dibromocarbazolyl triazole 5d displayed excellent inhibitory efficacy against most of the tested fungal strains (MIC = 2-32 μg/mL) and effectively fungicidal ability towards C. albicans, C. tropicals and C. parapsilosis ATCC 22019 (MFC = 4-8 μg/mL)...
June 15, 2018: European Journal of Medicinal Chemistry
Chris R Kenyon, Ilan S Schwartz
Contemporary strategies to curtail the emergence of antimicrobial resistance in Neisseria gonorrhoeae include screening for and treating asymptomatic infections in high-prevalence populations in whom antimicrobial drug-resistant infections have typically emerged. We argue that antimicrobial resistance in these groups is driven by a combination of dense sexual network connectivity and antimicrobial drug exposure (for example, through screen-and-treat strategies for asymptomatic N. gonorrhoeae infection). Sexual network connectivity sustains a high-equilibrium prevalence of N...
July 2018: Emerging Infectious Diseases
Tianyu Yu, Yue Jiang, Sijie Lin
The zebrafish is a globally recognized fresh water organism frequently used in developmental biology, environmental toxicology, and human disease related research fields. Thanks to its unique features, including large fecundity, embryo translucency, rapid and simultaneous development, etc., zebrafish embryos are often used for large scale toxicity assessment of chemicals and drug/compound screening. A typical screening procedure involves adult zebrafish spawning, embryos selection, and arraying the embryos into multi-well plates...
June 1, 2018: Journal of Visualized Experiments: JoVE
Aldo Tagliabue, Rino Rappuoli
Antimicrobial resistance (AMR) is currently the most alarming issue for human health. AMR already causes 700,000 deaths/year. It is estimated that 10 million deaths due to AMR will occur every year after 2050. This equals the number of people dying of cancer every year in present times. International institutions such as G20, World Bank, World Health Organization (WHO), UN General Assembly, European Union, and the UK and USA governments are calling for new antibiotics. To underline this emergency, a list of antibiotic-resistant "priority pathogens" has been published by WHO...
2018: Frontiers in Immunology
Chuan Zhou, Shichao Lai, Yong Xie, Shu Zhang, Yiping Lu
INTRODUCTION: Muscular symptoms, including stiffness, myalgia, cramps, and fatigue, are present in the majority of the patients with hypopituitarism, adrenal insufficiency and hypothyroidism, but rhabdomyolysis, the rapid breakdown of skeletal muscle, is a rare manifestation. In most patients who develop rhabdomyolysis, precipitating factors, such as strenuous exercise or use of lipid-lowering drugs, can be identified. CASE REPORT: We report the case of a 23-year-old male with primary hypopituitarism who developed acute renal impairment (AKI) with rhabdomyolysis after strenuous physical activity (push-ups)...
June 7, 2018: American Journal of Emergency Medicine
Sebastian Walther, Katharina Stegmayer
Diagnosis and treatment of motor phenomena in schizophrenia spectrum disorders Abstract. Motor abnormalities are intrinsic features of schizophrenia spectrum disorders. They may be spontaneous or antipsychotic drug-induced. The four most important symptom groups are abnormal involuntary movements or dyskinesia, Parkinsonism, catatonia and neurological soft signs. In addition, there are further motor abnormalities, which are less frequent and less operationalized. The suspected etiology of motor abnormalities is strongly associated with altered neurodevelopment...
June 2018: Therapeutische Umschau. Revue Thérapeutique
Bo Ding, Zhiyuan Wang, Jianjun Xie, Guangfeng Zeng, Wenrui Chen
Chinese tonic liquor is an important dietary supplement in daily use, but it often happens that illicitly adulterated drugs in Chinese tonic liquor could lead to food safety issues. In this survey an analytical method consisting of a liquid chromatography quadrupole time of flight mass spectrometer (LC-Q-TOF-MS), coupled with QuEChERS pretreatment, was established for identification of phosphodiesterase type 5 enzyme (PDE-5) inhibitors in Chinese tonic liquors. 86 PDE-5 inhibitors were qualitatively analyzed by employing information dependent acquisition mass spectrometry (IDA-MS) in comparison with the accurate mass of the protonated molecular ion, isotopic pattern, library and chemical formula...
June 18, 2018: Food Additives & Contaminants. Part B, Surveillance
Lubertus Bijlsma, Rubén Gil-Solsona, Félix Hernández, Juan Vicente Sancho
Synthetic cannabinoids (SCs) are consumed as legal alternative to cannabis and often allow passing drug-screening tests. Their rapid transience on the drug scene, combined with their mostly unknown metabolic profiles, creates a scenario with constantly moving analytical targets, making their monitoring and identification challenging. The development of fast screening strategies for SCs, not directly focused on their chemical structure, as an alternative to the commonly applied target acquisition methods, would be highly appreciated in forensic and public health laboratories...
June 16, 2018: Analytical and Bioanalytical Chemistry
Preet Kaur Sahota, Siri Shastry, Dana B Mukamel, Linda Murphy, Narisu Yang, Shahram Lotfipour, Bharath Chakravarthy
INTRODUCTION: The opioid drug epidemic is a major public health concern and an economic burden in the United States. The purpose of this systematic review is to assess the reliability and validity of screening instruments used in emergency medicine settings to detect opioid use in patients and to assess psychometric data for each screening instrument. METHODS: PubMed/MEDLINE, PsycINFO, Cochrane Database of Systematic Reviews, Cochrane Central Register of Controlled Trials, Web of Science, Cumulative Index to Nursing and Allied Health Literature and ClinicalTrials...
May 24, 2018: Addictive Behaviors
Rajiv Kumar, Lalit Vats, Silvia Bua, Claudiu T Supuran, Pawan K Sharma
In a quest to discover new biologically active compounds, a series of twenty novel heterocyclic derivatives substituted at position 5 with -H (7a-7j) or -CF3 (8a-8j), bearing benzenesulfonamide at N-1 position and various aroyl groups at position 4 of the 1,2,3-triazole ring was synthesized and screened for their carbonic anhydrase (CA, EC inhibition potential against four human (h) isoforms hCA I, II, IV and IX. All the compounds (7a-7j and 8a-8j) were synthesized via [3+2] cycloaddition reaction from 4-azidobenzenesulfonamide...
June 8, 2018: European Journal of Medicinal Chemistry
Mai I Shahin, Joyeeta Roy, Maha Hanafi, Dongyao Wang, Urarika Luesakul, Yifeng Chai, Nongnuj Muangsin, Deena S Lasheen, Dalal A Abou El Ella, Khaled A Abouzid, Nouri Neamati
No new and effective treatments have been approved for the treatment of esophageal squamous cell carcinoma (ESCC) in the past decade. Cisplatin and 5-fluoruracil are the most commonly used drugs for this disease. In order to develop a new class of drugs effective in our ESCC phenotypic screens, we began a systematic approach to generate novel compounds based on the 2-oxo-1,2-dihydroquinoline-4-carboxamide fragment. Herein, we report on the synthesis and initial assessment of 55 new analogues in two ESCC cell lines...
May 29, 2018: European Journal of Medicinal Chemistry
Felipe Borges Almeida, Alan Rios Fonseca, Núbia Heidrich, Maurício Schüler Nin, Helena Maria Tannhauser Barros
Depression is a highly incapacitating disorder known to have a multifactorial etiology, including a hereditary genetic background. The neurosteroid allopregnanolone (ALLO) is a positive allosteric modulator of the GABAA receptor and has been shown to have an antidepressant-like effect in animals. This study aimed to assess the behavioral effect of ALLO in animals with different backgrounds of depressive-like activity. An initial population (F0) of male and female Wistar rats was screened for immobility behavior utilizing the Forced Swim Test (FST)...
June 12, 2018: Physiology & Behavior
Andreas Zimmermann, Sebastian Hofer, Tobias Pendl, Katharina Kainz, Frank Madeo, Didac Carmona-Gutierrez
In the search for interventions against aging and age-related diseases, biological screening platforms are indispensable tools to identify anti-aging compounds among large substance libraries. The budding yeast, Saccharomyces cerevisiae, has emerged as a powerful chemical and genetic screening platform, as it combines a rapid workflow with experimental amenability and the availability of a wide range of genetic mutant libraries. Given the amount of conserved genes and aging mechanisms between yeast and human, testing candidate anti-aging substances in yeast gene-deletion or overexpression collections, or de novo derived mutants, has proven highly successful in finding potential molecular targets...
September 1, 2018: FEMS Yeast Research
Othman Soufan, Wail Ba-Alawi, Arturo Magana-Mora, Magbubah Essack, Vladimir B Bajic
High-throughput screening (HTS) performs the experimental testing of a large number of chemical compounds aiming to identify those active in the considered assay. Alternatively, faster and cheaper methods of large-scale virtual screening are performed computationally through quantitative structure-activity relationship (QSAR) models. However, the vast amount of available HTS heterogeneous data and the imbalanced ratio of active to inactive compounds in an assay make this a challenging problem. Although different QSAR models have been proposed, they have certain limitations, e...
June 14, 2018: Scientific Reports
Jeremiah Hadwen, Sarah Schock, Alan Mears, Robert Yang, Philippe Charron, Liying Zhang, Hualin S Xi, Alex MacKenzie
Rare monogenic diseases affect millions worldwide; although over 4,500 rare disease genotypes are known, disease-modifying drugs are available for only 5% of them. The sheer number of these conditions combined with their rarity precludes traditional costly drug discovery programs. An economically viable alternative is to repurpose established drugs for rare diseases. Many genetic diseases result from increased or decreased protein activity and identification of clinically approved drugs which moderate this pathogenic dosage holds therapeutic potential...
June 13, 2018: Human Molecular Genetics
Vladimir P Berishvili, Andrew E Voronkov, Eugene V Radchenko, Vladimir A Palyulin
One of the major challenges in the current drug discovery is the improvement of the docking-based virtual screening performance. It is especially important in the rational design of compounds with desired polypharmacology or selectivity profiles. To address this problem, we present a methodology for the development of target-specific scoring functions possessing high screening power. These scoring functions were built using the machine learning methods for the dual target inhibitors of PI3Kα and tankyrase, promising targets for colorectal cancer therapy...
June 14, 2018: Molecular Informatics
Mehmet Bulut, Muhammet Kazım Erol, Devrim Toslak, Melih Akidan, Ebru Kaya Başar, Hasan Fatih Çay
Objectives: This study aims to detect hydroxychloroquine (HCQ)-induced retinal toxicity at an earlier stage through the use of spectral-domain optical coherence tomography device, especially by measuring macular retinal ganglion cell-inner plexiform layer (RGC-IPL) thickness. Patients and methods: In this study, 92 eyes of 46 Caucasian female patients (mean age 53.6±8.1 years; range 32 to 69 years) who were taking HCQ were assigned to group 1, while 80 eyes of 40 age-matched Caucasian female control subjects (mean age 56...
March 2018: Archives of Rheumatology
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